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About This Item
Empirical Formula (Hill Notation):
C18H15N5O3
CAS Number:
Molecular Weight:
349.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
orange-red
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
N1C(=O)C(=C(C1=O)c3c4c([n](c3)CCCO)nccc4)c2nccnc2
InChI
1S/C18H15N5O3/c24-8-2-7-23-10-12(11-3-1-4-21-16(11)23)14-15(18(26)22-17(14)25)13-9-19-5-6-20-13/h1,3-6,9-10,24H,2,7-8H2,(H,22,25,26)
InChI key
ZDEJZKULWCZIHL-UHFFFAOYSA-N
General description
A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and ATP-competitive inhibitor of GSK-3β (Ki = 25 nM) and minimally inhibits a panel of 79 commonly studied protein kinases, including several PKC isozymes. Shown to increase intracellular glycogen synthase activity in HEK293 cells with an EC50 of 32 nM and demonstrate metabolic stability in human liver microsomes (HLM; t1/2 >100 min).
A cell-permeable, potent, specific, and ATP-competitive inhibitor of GSK-3β (Ki = 25 nM) that exhibits minimal inhibition against a panel of 79 commonly studied protein kinases, including several PKC isozymes. Shown to increase intracellular glycogen synthase activity in HEK293 cells (EC50 = 32 nM) and demonstrate metabolic stability in human liver microsomes (HLM; t1/2 >100 min).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Gsk-3β
Gsk-3β
Product competes with ATP.
Reversible: no
Target Ki: 25 nM against GSK-3β
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Justman, Q.A., et al. 2009. Science324, 509.
O′Neill, D.J., et al. 2004. Bioorg. Med. Chem.12, 3167.
O′Neill, D.J., et al. 2004. Bioorg. Med. Chem.12, 3167.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
Storage Class
11 - Combustible Solids
wgk
WGK 1
Certificates of Analysis (COA)
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Seda Mehtap Sarı Kılıçaslan et al.
Iranian journal of basic medical sciences, 24(11), 1500-1508 (2022-03-24)
This study examines the impact of integrin-linked kinase (ILK), protein kinase B (AKT), glycogen synthase kinase-3β (GSK-3β), and β-catenin signal molecules in SKOV-3 ovarian cancer cells adhered to fibronectin. Expression levels of α4, αv, β1, and β6 integrin subunits known
Global Trade Item Number
| SKU | GTIN |
|---|---|
| 361553-1MG | 04055977214116 |